CA2423050A1 - Derives de pyrazine tenant lieu de modulateurs de tyrosine kinase - Google Patents
Derives de pyrazine tenant lieu de modulateurs de tyrosine kinase Download PDFInfo
- Publication number
- CA2423050A1 CA2423050A1 CA002423050A CA2423050A CA2423050A1 CA 2423050 A1 CA2423050 A1 CA 2423050A1 CA 002423050 A CA002423050 A CA 002423050A CA 2423050 A CA2423050 A CA 2423050A CA 2423050 A1 CA2423050 A1 CA 2423050A1
- Authority
- CA
- Canada
- Prior art keywords
- amino
- alkyl
- group
- compound
- mmol
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Pain & Pain Management (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
L'invention concerne des dérivés de pyrazine inhibant l'activité de tyrosine kinase. Certains de ces dérivés sont des inhibiteurs sélectifs de tyrosine kinase du récepteur de facteur de croissance endothéliale. L'invention concerne également des formulations pharmaceutiques renfermant les dérivés décrits et des procédés relatifs à l'utilisation des formulations considérées comme agents antitumoraux et dans le traitement des cancers à tumeur solide, de l'angiogenèse, de la rétinopathie diabétique, de la polyarthrite rhumatoïde, de l'endométriose et du psoriasis.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23396800P | 2000-09-20 | 2000-09-20 | |
| US60/233,968 | 2000-09-20 | ||
| PCT/US2001/029175 WO2002024681A2 (fr) | 2000-09-20 | 2001-09-19 | Derives de pyrazine tenant lieu de modulateurs de tyrosine kinase |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2423050A1 true CA2423050A1 (fr) | 2002-03-28 |
Family
ID=22879359
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002423050A Abandoned CA2423050A1 (fr) | 2000-09-20 | 2001-09-19 | Derives de pyrazine tenant lieu de modulateurs de tyrosine kinase |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US6710048B2 (fr) |
| EP (1) | EP1330452B1 (fr) |
| JP (1) | JP2004523474A (fr) |
| AR (1) | AR035494A1 (fr) |
| AT (1) | ATE415396T1 (fr) |
| AU (1) | AU9458401A (fr) |
| CA (1) | CA2423050A1 (fr) |
| DE (1) | DE60136731D1 (fr) |
| DK (1) | DK1330452T3 (fr) |
| ES (1) | ES2315308T3 (fr) |
| HK (1) | HK1054393B (fr) |
| PT (1) | PT1330452E (fr) |
| TW (1) | TWI254711B (fr) |
| WO (1) | WO2002024681A2 (fr) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040077605A1 (en) * | 2001-06-20 | 2004-04-22 | Salvati Mark E. | Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function |
| EP1854798A3 (fr) * | 2000-09-19 | 2007-11-28 | Bristol-Myers Squibb Company | Composés de succinimide hétérocyclique fondu et leurs analogies, modulateurs de la fonction de récepteur d'hormone nucléaire |
| US20040087548A1 (en) | 2001-02-27 | 2004-05-06 | Salvati Mark E. | Fused cyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function |
| DE60228330D1 (de) * | 2001-12-19 | 2008-09-25 | Bristol Myers Squibb Co | Kondensierte heterocyclische verbindungen und deren analoga; modulatoren der funktion von nukleären hormonrezeptoren |
| US7482366B2 (en) * | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| EP1501514B1 (fr) * | 2002-05-03 | 2012-12-19 | Exelixis, Inc. | Modulateurs de proteine-kinases et leurs methodes d'utilisation |
| AUPS251502A0 (en) * | 2002-05-23 | 2002-06-13 | Cytopia Pty Ltd | Protein kinase inhibitors |
| AUPS251402A0 (en) * | 2002-05-23 | 2002-06-13 | Cytopia Pty Ltd | Kinase inhibitors |
| US7015227B2 (en) * | 2002-06-21 | 2006-03-21 | Cgi Pharmaceuticals, Inc. | Certain amino-substituted monocycles as kinase modulators |
| GB0215775D0 (en) * | 2002-07-06 | 2002-08-14 | Astex Technology Ltd | Pharmaceutical compounds |
| US20060293256A1 (en) * | 2002-08-06 | 2006-12-28 | Masateru Yamada | Remedy or preventive for kidney disease and method of diagnosing kidney disease |
| SI1569907T1 (sl) * | 2002-12-13 | 2016-06-30 | Ym Biosciences Australia Pty Ltd | Na nikotinamidu osnovani kinazni inhibitorji |
| US20040121968A1 (en) * | 2002-12-23 | 2004-06-24 | Alexander Ljubimov | Antiangiogenesis by inhibiting protein kinase CK2 activity |
| CA2517256C (fr) * | 2003-02-26 | 2013-04-30 | Sugen, Inc. | Composes d'aminoheteroaryle utilises en tant qu'inhibiteurs de proteine kinase |
| GB2400101A (en) * | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| CA2530389A1 (fr) * | 2003-07-02 | 2005-01-13 | Biofocus Discovery Limited | Composes se liant au site actif d'enzymes proteine kinases |
| AU2004278382B2 (en) * | 2003-09-30 | 2008-09-18 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| JP2007512275A (ja) * | 2003-11-24 | 2007-05-17 | エフ.ホフマン−ラ ロシュ アーゲー | ピラゾリルおよびイミダゾリルピリミジン |
| WO2005058876A1 (fr) * | 2003-12-16 | 2005-06-30 | Gpc Biotech Ag | Derives de la pyrazine utilises en tant que composes efficaces contre les maladies infectieuses |
| ATE481134T1 (de) | 2004-01-21 | 2010-10-15 | Univ Emory | Zusammensetzungen und verwendung von tyrosinkinase-hemmern zur behandlung von pathogenen infektionen |
| EP1814856A1 (fr) * | 2004-11-12 | 2007-08-08 | Galapagos N.V. | Composés hétéroaromatiques de l'azote qui se lient au site actif d'enzymes de type protéines kinases |
| GB0428082D0 (en) * | 2004-12-22 | 2005-01-26 | Welcome Trust The Ltd | Therapeutic compounds |
| GB0500226D0 (en) * | 2005-01-07 | 2005-02-16 | Biofocus Discovery Ltd | Compounds which bind to the active site of protein kinase enzymes |
| KR100674813B1 (ko) * | 2005-08-05 | 2007-01-29 | 일양약품주식회사 | N-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 |
| EP1917244A2 (fr) | 2005-08-24 | 2008-05-07 | Abbott GmbH & Co. KG | Composes guanidine a substitution hetaryl et utilisation en tant que partenaires de liaison pour des recepteurs de 5-ht5 |
| GT200600411A (es) * | 2005-09-13 | 2007-05-21 | Novartis Ag | Combinaciones que comprenden un inhibidor del receptor del factor de crecimiento endotelial vascular |
| WO2008070350A2 (fr) * | 2006-10-27 | 2008-06-12 | The Board Of Regents Of The University Of Texas System | Procédés et compositions liés aux enveloppements de déshydrons |
| WO2008138992A1 (fr) * | 2007-05-16 | 2008-11-20 | Bayer Cropscience Sa | Dérivés fongicides phényl-pyrimidinyl-amino |
| WO2009037247A1 (fr) * | 2007-09-17 | 2009-03-26 | Neurosearch A/S | Dérivés de pyrazine et leur utilisation en tant que modulateurs des canaux potassiques |
| KR100898037B1 (ko) * | 2007-10-05 | 2009-06-01 | 한국화학연구원 | 금속촉매의 커플링반응에 의한 트리알킬피라진 유도체의제조방법 |
| US8716317B2 (en) | 2008-06-09 | 2014-05-06 | Sanofi | Sulfonamides with heterocycle and oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals |
| US20110112121A1 (en) * | 2009-07-06 | 2011-05-12 | Joerg Berghausen | Pharmaceutical Compositions and Solid Forms |
| US8415381B2 (en) * | 2009-07-30 | 2013-04-09 | Novartis Ag | Heteroaryl compounds and their uses |
| KR101906146B1 (ko) * | 2009-08-17 | 2018-10-10 | 메모리얼 슬로안-케터링 캔서 센터 | 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법 |
| US20120165306A1 (en) * | 2009-09-04 | 2012-06-28 | Barsanti Paul A | Pyrazinylpyridines useful for the treatment of proliferative diseases |
| US20110185353A1 (en) * | 2010-01-27 | 2011-07-28 | Jack Matthew | Mitigating Problems Arising From Incompatible Software |
| JP2013542967A (ja) * | 2010-11-17 | 2013-11-28 | ノバルティス アーゲー | 3−(アミノアリール)−ピリジン化合物 |
| JP2014506878A (ja) * | 2011-01-28 | 2014-03-20 | ノバルティス アーゲー | Cdk9阻害剤としての置換ビ−ヘテロアリール化合物およびそれらの使用 |
| JP6116554B2 (ja) * | 2011-07-07 | 2017-04-19 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | がんの処置のための置換されたアザ複素環 |
| KR20220143164A (ko) | 2012-11-21 | 2022-10-24 | 피티씨 테라퓨틱스, 인크. | 치환된 리버스 피리미딘 bmi-1 저해제 |
| AR093580A1 (es) | 2013-08-30 | 2015-06-10 | Ptc Therapeutics Inc | Inhibidores bmi-1 de pirimidina sustituidos |
| WO2015076800A1 (fr) * | 2013-11-21 | 2015-05-28 | Ptc Therapeutics, Inc. | Inhibiteurs de bmi-1 à base de pyridine et de pyrazine substituées |
| KR102461419B1 (ko) | 2014-05-13 | 2022-11-02 | 메모리얼 슬로안 케터링 캔서 센터 | Hsp70 조정물질 및 이의 제조 및 이용 방법 |
| JP7249950B2 (ja) | 2017-03-27 | 2023-03-31 | カーデュリオン・ファーマシューティカルズ・リミテッド・ライアビリティ・カンパニー | ヘテロ環化合物 |
| GB201715414D0 (en) * | 2017-09-22 | 2017-11-08 | Syngenta Participations Ag | Improvements in or relating to organic compounds |
| GB201715318D0 (en) | 2017-09-22 | 2017-11-08 | Syngenta Participations Ag | Improvements in or relating to organic compounds |
| CN113164479A (zh) | 2018-08-17 | 2021-07-23 | Ptc医疗公司 | 用于治疗胰腺癌的方法 |
| IL281765B2 (en) | 2018-09-25 | 2024-04-01 | Cardurion Pharmaceuticals Inc | Aminopyrimidine compound |
| PT4182308T (pt) | 2020-07-15 | 2024-12-04 | Chiesi Farm Spa | Derivados de piridazinil amino como inibidores de alk5 |
| TW202229273A (zh) | 2020-09-28 | 2022-08-01 | 美商卡都瑞恩醫藥有限責任公司 | 稠合雜芳基化合物及其作為CaMKII抑制劑之用途 |
| AU2022351219A1 (en) | 2021-09-21 | 2024-05-02 | Chiesi Farmaceutici S.P.A. | Pyridazinyl amino derivatives as alk5 inhibitors |
| EP4463448A1 (fr) | 2022-01-11 | 2024-11-20 | Chiesi Farmaceutici S.p.A. | Dérivés pyridazinyl amino utilisés en tant qu'inhibiteurs d'alk5 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4514400A (en) * | 1981-10-26 | 1985-04-30 | William H. Rorer, Inc. | Cardiotonic 5-heteroaryl-pyridone |
| DE4426346A1 (de) * | 1994-07-25 | 1996-02-01 | Basf Ag | Herbizide Pyrazinderivate |
| GB9514160D0 (en) * | 1994-07-25 | 1995-09-13 | Zeneca Ltd | Aromatic compounds |
| PT994875E (pt) | 1997-06-30 | 2004-06-30 | Targacept Inc | Derivados de 3-piridil-1-aza-biciclo-alcano para a prevencao e tratamento de desordens do snc |
| JP2002519348A (ja) * | 1998-06-30 | 2002-07-02 | イーライ・リリー・アンド・カンパニー | 5−ht1fアゴニスト |
| EP1219609B1 (fr) * | 1999-09-16 | 2007-04-04 | Tanabe Seiyaku Co., Ltd. | Composes cycliques aromatiques azotes a six elements |
| CN1231473C (zh) | 2000-02-16 | 2005-12-14 | 神经能质公司 | 取代的芳基吡嗪 |
-
2001
- 2001-09-19 CA CA002423050A patent/CA2423050A1/fr not_active Abandoned
- 2001-09-19 PT PT01975243T patent/PT1330452E/pt unknown
- 2001-09-19 DK DK01975243T patent/DK1330452T3/da active
- 2001-09-19 DE DE60136731T patent/DE60136731D1/de not_active Expired - Lifetime
- 2001-09-19 WO PCT/US2001/029175 patent/WO2002024681A2/fr not_active Ceased
- 2001-09-19 EP EP01975243A patent/EP1330452B1/fr not_active Revoked
- 2001-09-19 AT AT01975243T patent/ATE415396T1/de not_active IP Right Cessation
- 2001-09-19 JP JP2002529091A patent/JP2004523474A/ja active Pending
- 2001-09-19 HK HK03106746.1A patent/HK1054393B/en not_active IP Right Cessation
- 2001-09-19 ES ES01975243T patent/ES2315308T3/es not_active Expired - Lifetime
- 2001-09-19 US US09/955,780 patent/US6710048B2/en not_active Expired - Lifetime
- 2001-09-19 AU AU9458401A patent/AU9458401A/xx active Pending
- 2001-09-20 AR ARP010104452A patent/AR035494A1/es not_active Application Discontinuation
-
2002
- 2002-09-05 TW TW091120227A patent/TWI254711B/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| TWI254711B (en) | 2006-05-11 |
| WO2002024681A3 (fr) | 2002-06-20 |
| EP1330452B1 (fr) | 2008-11-26 |
| AR035494A1 (es) | 2004-06-02 |
| HK1054393B (en) | 2009-08-28 |
| JP2004523474A (ja) | 2004-08-05 |
| WO2002024681A2 (fr) | 2002-03-28 |
| US6710048B2 (en) | 2004-03-23 |
| HK1054393A1 (en) | 2003-11-28 |
| PT1330452E (pt) | 2009-01-22 |
| AU9458401A (en) | 2002-04-02 |
| US20030060629A1 (en) | 2003-03-27 |
| EP1330452A2 (fr) | 2003-07-30 |
| DE60136731D1 (de) | 2009-01-08 |
| ATE415396T1 (de) | 2008-12-15 |
| DK1330452T3 (da) | 2009-03-16 |
| ES2315308T3 (es) | 2009-04-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Discontinued |